Use of sodium octenyl-succinate starches as a binder in continuous wet granulation

Abstract

The present invention relates to the use of sodium octenyl succinate starch as a binder in twin screw granulation, in particular for pharmaceutical solid dosage form and the granule obtainable by the method thereof.

1 - 17 . (canceled) 
     
     
         18 . A method for preparing granules comprising one or several substances by continuous wet granulation comprising the steps of:
 a) feeding substance powder to a continuous wet granulator;   b) feeding a granulation liquid to said continuous wet granulator,   c) wetting the substance powder with the granulation liquid in presence of a binder consisting of an octenyl succinate starch in order to obtain said granules and d) drying said granules.   
     
     
         19 . The method of  claim 18  wherein said continuous wet granulation is extrusion granulation, preferably twin screw granulation. 
     
     
         20 . The method of  claim 18  comprising the steps of:
 a1) mixing substance powder with powder of said binder, 
 a2) feeding said powder mixture to a continuous wet granulator, 
 b) feeding a granulation liquid consisting of a solvent to said continuous wet granulator, 
 c) wetting the powder mixture with the solvent in order to obtain said granules, 
 d) drying said granules. 
 
     
     
         21 . The method of  claim 18  comprising the steps of:
 a) feeding said substance powder to a continuous wet granulator, 
 b) feeding a granulation liquid comprising said binder to said continuous wet granulator, 
 c) wetting the substance powder with the granulation liquid in order to obtain said granules, 
 d) drying said granules. 
 
     
     
         22 . The method according to  claim 18  wherein said octenyl succinate has a weight average molecular weight comprised between 10 4  and 10 7  g/mol, preferably 10 4  and 10 6  g/mol, more preferably 10 5  and 10 6  g/mol. 
     
     
         23 . The method of  claim 22 , wherein said octenyl succinate has a weight average molecular weight comprised between 100 000 and 500 000 g/mol, preferably 100 000 and 400 000 g/mol, still preferably 100 000 and 300 000 g/mol, still preferably 100 000 and 200 000 g/mol, still again more preferably 150 000 g/mol. 
     
     
         24 . The method of  claim 22 , wherein said octenyl succinate has a weight average molecular weight comprised between 300 000 and 10 6  g/mol, more preferably 400 000 to 900 000 g/mol, still preferably 500 000 to 800 000 g/mol, still preferably 550 000 to 750 000 g/mol, more preferably 600 000 g/mol. 
     
     
         25 . The method according to  claim 18  further comprising a step e) of milling the dried granules. 
     
     
         26 . The method according to  claim 18  wherein said octenyl succinate starch is a waxy maize octenyl succinate starch. 
     
     
         27 . The method according to  claim 18  wherein said octenyl succinate starch content is between 1 and 50%, preferably 1 and 15% by weight of the total dry weight of said granules. 
     
     
         28 . The method according to  claim 18  wherein said substance is a pharmaceutical active agent. 
     
     
         29 . A method for preparing pharmaceutical tablets comprising the steps of preparing granules according to  claim 18  and a final step of compressing the granules in order to obtain tablets. 
     
     
         30 . A granule comprising one or several substances and an octenyl succinate starch having a weight average molecular weight comprised between 10 4  and 10 7  g/mol, preferably 10 4  and 10 6  g/mol, more preferably 10 5  and 10 6  g/mol. 
     
     
         31 . The granule of  claim 30 , wherein said octenyl succinate has a weight average molecular weight comprised between 100 000 and 500 000 g/mol, preferably 100 000 and 400 000 g/mol, still preferably 100 000 and 300 000 g/mol, still preferably 100 000 and 200 000 g/mol, still again more preferably 150 000 g/mol. 
     
     
         32 . The granule of  claim 30 , wherein said octenyl succinate has a weight average molecular weight comprised between 300 000 and 10 6  g/mol, more preferably 400 000 to 900 000 g/mol, still preferably 500 000 to 800 000 g/mol, still preferably 550 000 to 750 000 g/mol, more preferably 600 000 g/mol. 
     
     
         33 . A pharmaceutical tablet comprising a granule according to  claim 30 . 
     
     
         34 . Use of octenyl succinate as a binder for continuous wet granulation.